Pharmacokinetics of tetrahydroaminoacridine: Relations to clinical and biochemical effects in Alzheimer patients

A. Åhlin, A. Adem, T. Junthé, G. Öhman, H. Nybäck

Research output: Contribution to journalArticlepeer-review

42 Scopus citations

Abstract

The pharmacokinetics of tetrahydroaminoacridine (THA) was studied in patients suffering from Alzheimer's dementia. Single doses of the drug were administered by intravenous (15 mg), oral (50 mg) and rectal routes (25 mg). Pharmacokinetic parameters were related to clinical and biochemical effects in patients who, in a separate study, participated in a clinical trial of oral THA. The bioavailability of THA was low and varied considerably between subjects. Clinical improvement and occurrence of elevated liver enzymes correlated positively with drug bioavailability. Acetyl and buturyl cholinesterase activities in the plasma did not change following THA administration. Rectally administered THA had a higher bioavailability than orally administered THA in three subjects who were given the drug by both routes. These results indicate that a clinical trial of rectal THA would be justified as this administration route may improve resorption and diminish first-pass metabolism of the drug in the liver compared with oral administration.

Original languageBritish English
Pages (from-to)29-36
Number of pages8
JournalInternational Clinical Psychopharmacology
Volume7
Issue number1
DOIs
StatePublished - 1992

Fingerprint

Dive into the research topics of 'Pharmacokinetics of tetrahydroaminoacridine: Relations to clinical and biochemical effects in Alzheimer patients'. Together they form a unique fingerprint.

Cite this